The present inventors synthesized 3-amido-1,2-benzoisoxazole derivatives represented by the following formula 2 while they synthesized compounds of various structures and verified their efficiency as antagonists against the Leukotriene-B-4 (hereinafter referred to as LTB-4) receptor and their osteogenesis stimulation effect in order to treat various diseases related to LTB-4. It has been found out that compounds of the following formula 2 have simultaneous efficiency in showing antagonism against the LTB-4 receptor and in stimulating osteogenesis (Korea Patent Application No. 1998-71076A; U.S. Pat. No. 6,150,390). However, they also have a disadvantage that they are inadequate to be used as a drug since the bioavailability is not so good.

(wherein, n is an integer of 3 to 5.)
Hereupon, the present inventors synthesized novel 3-amido-1,2-benzoisoxazole derivatives represented by formula 1 of the present invention by introducing amino acid residue to the amine group of a 3-amido-1,2-benzoisoxazole in order to improve the bioavailability of compounds of the above formula 2. In addition, they completed this invention by finding out that compounds of the present invention not only showed efficiency as antagonists against LTB-4 receptor, inhibitors of osteolysis and stimulators of osteogenesis but also increased solubility in water and improved bioavailability by having high absorption ratio in vivo, and thus, improved their medical effect.